陈妍, 邓英杰, 郝艳丽, 王振远, 盛军. 心肌细胞靶向脂质体的制备及体外靶向性研究J. 药学学报, 2005, 40(6): 568-572.
引用本文: 陈妍, 邓英杰, 郝艳丽, 王振远, 盛军. 心肌细胞靶向脂质体的制备及体外靶向性研究J. 药学学报, 2005, 40(6): 568-572.
CHEN Yan, DENG Ying-jie, HAO Yan-li, WANG Zhen-yuan, SHENG Jun. Preparation of cardiomyocyte-targeting liposomes and their targeting ability in virtoJ. Acta Pharmaceutica Sinica, 2005, 40(6): 568-572.
Citation: CHEN Yan, DENG Ying-jie, HAO Yan-li, WANG Zhen-yuan, SHENG Jun. Preparation of cardiomyocyte-targeting liposomes and their targeting ability in virtoJ. Acta Pharmaceutica Sinica, 2005, 40(6): 568-572.

心肌细胞靶向脂质体的制备及体外靶向性研究

Preparation of cardiomyocyte-targeting liposomes and their targeting ability in virto

  • 摘要: 目的制备心肌细胞靶向脂质体,并对其体外心肌细胞靶向性进行研究。方法选用与β1-受体阻滞剂艾司洛尔结构类似的亲脂性化合物PAC修饰脂质体(PAC-L);将荧光标记的普通脂质体(Plain-L)与PAC-L加入体外培养的心肌细胞中,在特定实验条件下共同培养一定时间后,用荧光分光光度计测定心肌细胞摄取荧光脂质体的量。结果PAC-L与心肌细胞有较强的亲和力,且心肌细胞对PAC-L的摄取显著高于非心肌细胞(P<0.001);常氧条件下2 h心肌细胞对PAC-L的摄取较Plain-L高约2.9倍,而在缺氧条件下则高出5.2倍;心肌细胞对Plain-L的摄取约11%是以内吞方式摄取的,而对PAC-L则约有56%是以内吞方式进行的。结论本文制备的PAC-L具有较强的心肌细胞特异靶向性,有可能成为一种有效的缺血心肌靶向性药物载体。

     

    Abstract: AimTo prepare the cardiomyocyte-targeting liposomes and investigate their cardiomyocyte targetability in virto. MethodsLiposomes modified with compound PAC were prepared (PAC-L); The uptake of PAC-L by cardiomyocytes was studied by incubating fluorescence labeled liposomes with cardiomyocytes in virto and measuring the association of liposomes by a fluorescence spectrophotometer. ResultsA high affinity of PAC-L to the cardiomyocytes was observed, the amount of cell uptake of PAC-L by cardiomyocytes was higher than that by nonmyocyte (P<0.001); The amount of cardiomyocyte uptake of PAC-L on the normoxia condition 2 h was 2.9-fold higher than that of plain-L, and the increase was 5.2-fold when hypoxia occured; The form of liposome uptake changed, the amount of cardiomyocyte uptake of Plain-L by internalization was only 11%, while that of PAC-L was 56%. ConclusionIt is indicated that PAC-L was a potential drug carrier for targeting to ischemic myocardium.

     

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